Articles producció científica> Química Analítica i Química Orgànica

Bridgehead Modifications of Englerin A Reduce TRPC4 Activity and Intravenous Toxicity but not Cell Growth Inhibition

  • Identification data

    Identifier: imarina:9296648
  • Authors:

    Wu, Zhenhua
    Suppo, Jean-Simon
    Tumova, Sarka
    Strope, Jonathan
    Bravo, Fernando
    Moy, Melody
    Weinstein, Ethan S.
    Peer, Cody J.
    Figg, William D.
    Chain, William J.
    Echavarren, Antonio M.
    Beech, David J.
    Beutler, John A.
  • Others:

    Author, as appears in the article.: Wu, Zhenhua; Suppo, Jean-Simon; Tumova, Sarka; Strope, Jonathan; Bravo, Fernando; Moy, Melody; Weinstein, Ethan S.; Peer, Cody J.; Figg, William D.; Chain, William J.; Echavarren, Antonio M.; Beech, David J.; Beutler, John A.;
    Department: Química Analítica i Química Orgànica
    URV's Author/s: BRAVO LARA, FERNANDO / ECHAVARREN PABLOS, ANTONIO
    Keywords: Trpc4 Tonantzitlolone Pkc-theta Mice Kidney cancer Ion channels Formal synthesis Englerin Cytotoxicity Channels Biological evaluation (-)-englerin
    Abstract: Modifications at the bridgehead position of englerin A were made to explore the effects of variation at this site on the molecule for biological activity, as judged by the NCI 60 screen, in which englerin A is highly potent and selective for renal cancer cells. Replacement of the isopropyl group by other, larger substituents yielded compounds which displayed excellent selectivity and potency comparable to the natural product. Selected compounds were also evaluated for their effect on the ion channel TRPC4 as well as for intravenous toxicity in mice, and these had lower potency in both assays compared to englerin A.
    Thematic Areas: Química Organic chemistry Medicina ii Medicina i Materiais Interdisciplinar Farmacia Drug discovery Ciências biológicas iii Ciências biológicas ii Ciências biológicas i Chemistry, medicinal Biotecnología Biochemistry
    licence for use: https://creativecommons.org/licenses/by/3.0/es/
    Author's mail: antoniomaria.echavarren@urv.cat
    Author identifier: 0000-0002-6418-7930
    Record's date: 2024-01-14
    Papper version: info:eu-repo/semantics/acceptedVersion
    Link to the original source: https://pubs.acs.org/doi/10.1021/acsmedchemlett.0c00186
    Papper original source: Acs Medicinal Chemistry Letters. 11 (9): 1711-1716
    APA: Wu, Zhenhua; Suppo, Jean-Simon; Tumova, Sarka; Strope, Jonathan; Bravo, Fernando; Moy, Melody; Weinstein, Ethan S.; Peer, Cody J.; Figg, William D.; C (2020). Bridgehead Modifications of Englerin A Reduce TRPC4 Activity and Intravenous Toxicity but not Cell Growth Inhibition. Acs Medicinal Chemistry Letters, 11(9), 1711-1716. DOI: 10.1021/acsmedchemlett.0c00186
    Licence document URL: https://repositori.urv.cat/ca/proteccio-de-dades/
    Article's DOI: 10.1021/acsmedchemlett.0c00186
    Entity: Universitat Rovira i Virgili
    Journal publication year: 2020
    Publication Type: Journal Publications
  • Keywords:

    Biochemistry,Chemistry, Medicinal,Drug Discovery,Organic Chemistry
    Trpc4
    Tonantzitlolone
    Pkc-theta
    Mice
    Kidney cancer
    Ion channels
    Formal synthesis
    Englerin
    Cytotoxicity
    Channels
    Biological evaluation
    (-)-englerin
    Química
    Organic chemistry
    Medicina ii
    Medicina i
    Materiais
    Interdisciplinar
    Farmacia
    Drug discovery
    Ciências biológicas iii
    Ciências biológicas ii
    Ciências biológicas i
    Chemistry, medicinal
    Biotecnología
    Biochemistry
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